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Tubulin polymerization-IN-41

CAS No. : 2804026-81-9

MCE 站：Tubulin polymerization-IN-41

产品活性：Tubulin polymerization-IN-41 是一种有效的微管蛋白聚合 (tubulin polymerization) 抑制剂，IC₅₀ 为 2.61 μM。Tubulin polymerization-IN-41 靶向微管蛋白的秋水仙碱结合位点。Tubulin polymerization-IN-41 具有抗癌作用。

研究领域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis

作用靶点：Microtubule/Tubulin  |  Apoptosis

In Vitro: Tubulin polymerization-IN-41 (compound C3) displays remarkable antiproliferative activities with IC₅₀ values of 6.3 nM, 9.2 nM, 8.3 nM, ａnd 8.7 nM for K562, MCF-7, HT29, ａnd HCT116 cells, respectively. Additionally, Tubulin polymerization-IN-41 shows marked activity against Paclitaxel-resistant MCF-7 cells ａnd A549 cells.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM) downregulates the expression of acetyl-α-tubulin (Ac-α-tubulin) ａnd upregulated the expression of detyrosinated-α-tubulin (DeY-α-tubulin) in a concentration-dependent manner.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) could arrest cancer cells in the G2/M phase, ａnd induces MCF-7 cells apoptosis in a concentration-dependent manner.
Tubulin polymerization-IN-41 (compound C3; 5-20 nM; 24 hours) reduces Ser216 phosphorylation, resulting in cdc2 Tyr15 dephosphorylation ａnd Thr161 phosphorylation, which ultimately leads to the activation of subsequent cdc2/cyclin B1 complex.

In Vivo: Tubulin polymerization-IN-41 (compound C3; 5-20 mg/kg; i.p; every two days; for 21 consecutive days) exhibits the significant potency of tumor growth inhibition in a dose dependence without weight loss in the drug-treated period.

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